Short peptide with an inhibitory activity on the NMDA/Gly-induced currents

D. S. Karlov, O. I. Barygin, M. Y. Dron, V. A. Palyulin, V. V. Grigoriev, M. V. Fedorov

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    1 Citation (Scopus)

    Abstract

    N-methyl-D-aspartate (NMDA) receptors are considered to be one of the most promising targets for treatment-resistant depression. The majority of known ligands may cause undesirable side-effects, except tetrapeptide rapastinel which demonstrated rapid antidepressant effect without psychotomimetic side effects. High shape similarity was noticed between dipeptide Phe-Tyr and NMDA receptor non-competitive antagonist ifenprodil which imply the possibility for antagonistic action of this peptide. A series of analogs were selected based on the docking results and molecular dynamics simulations. A dipeptide D-Phe-L-Tyr showed modest inhibitory activity comparable to rapastinel.

    Original languageEnglish
    Pages (from-to)683-695
    Number of pages13
    JournalSAR and QSAR in Environmental Research
    Volume30
    Issue number9
    DOIs
    Publication statusPublished - 2 Sep 2019

    Keywords

    • glutamate receptors
    • molecular dynamics simulations
    • Neuroactive peptides
    • patch clamp
    • radioligand studies

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